In vitro permeation through porcine buccal mucosa of caffeic acid phenetyl ester (CAPE) from a topical mucoadhesive gel containing propolis

Recent studies have shown that propolis has on the oral cavity appreciable antibacterial, antifungal and antiviral actions, as well as anti-inflammatory, anaesthetic and cytostatic properties. In light of these studies, an assessment of the diffusion and permeation of caffeic acid phenetyl ester (CAPE) through porcine buccal mucosa was considered useful as a possible application in the stomatological field. To do so, a mucoadhesive topical gel was prepared to apply to the buccal mucosa. The gel was formulated in such a way as to improve the solubility of the propolis, conducting to an increase of the flux. The mucosal permeation of CAPE from the formulation was evaluated using Franz cells, with porcine buccal mucosa as septum between the formulation (donor compartment) and the receptor phase chamber. The diffusion through the membrane was determined by evaluating the amount of CAPE present in the receiving solution, the flux and the permeation coefficient (at the steady state) in the different formulations at set intervals. Qualitative and quantitative determinations were done by HPLC analysis. From the results, CAPE allowed a high permeability coefficient in comparison to the coefficient of other molecules, as expected from its physical-chemical structure. Moreover, the developed gel improved the CAPE flux approximately 35 times more with respect to an ethanol solution formulated at the same gel concentration. The developed gel was also tested in order to evaluate the mucoadhesive behaviour and comfort in vivo on 10 volunteers in a period of 8 h. The in vivo evaluation of mucoadhesive gel revealed adequate comfort and non-irritancy during the period of study and it was well accepted by the volunteers.     

Characterization of a cinnamoyl derivative from broccoli (Brassica oleracea L. var. italica) florets

A new intact glucosinolate Cinnamoyl derivative [6'-O-trans-(4″- hydroxy cinnamoyl)-4-(methylsulphinyl) butyl glucosinolate] (A) has been isolated from Broccoli (Brassica oleracea L. var. italica) florets. The compound was isolated and characterized by LC, MS-ESI, FTIR, ¹H and ¹³C NMR as well as ¹H-¹H COSY, DEPT 135° spectrometric experiments.     

Insecticidal activity of (2<Emphasis Type="Italic">n</Emphasis>-octyl<Emphasis Type="Italic">cyclo</Emphasis>prop-1-enyl)-octanoic acid (I) against three Coleopteran stored product insects from <Emphasis Type="Italic">Sterculia foetida</Emphasis> (L.)

The insecticidal activities of the extracts, fractions, and pure compound of Sterculia foetida (L.) seeds were investigated against three major stored product pests, namely, Sitophilus oryzae (L.), Callosobruchus chinensis (L.), and Tribolium castaneum (H.), through contact and fumigation bioassay. Responses varied with test chemicals, insect species, exposure times, and doses individually. The biologically active constituent of the S. foetida seeds was characterized as a cyclopropene fatty acid structurally elucidated as (2n-octylcycloprop-1-enyl)-octanoic acid (I) by spectroscopic analysis. The filter paper application of, (2n-octylcycloprop-1-enyl)-octanoic acid (I) at 0.2 mg/cm² caused 100% mortality to all test insects 2 days after treatment (2 DAT). Among the chromatographic fractions, only the pure hexane-eluted fraction caused 100% mortality at 0.3 mg/cm² to S. oryzae and C. chinensis 2 DAT, while the dose required to obtain the same percentage of mortality with the crude seed extract was 0.6 mg/cm². Under all treatment conditions, T. castaneum exhibited less susceptibility, taking longer than the other insects to show symptoms of toxicity. In terms of fumigant activity, the compounds appeared to be more effective in a vapor form against all the three insects in closed containers compared with open containers. These results suggest that the insecticidal activities of the test compounds were attributable to contact mode of action, although there was also significant fumigant toxicity. The results indicate that the bioactive compound isolated from S. foetida could act as a potent insecticide against S. oryzae, C. chinensis, and T. castaneum populations.